Enzyme Modulators

<p>Inhibits type III tyrosine kinases (PDGFRα, PDGFRβ, FLT3)</p>

<p>A reversible inhibitor of IGF-1R kinase and insulin receptor. Has anti-growth effects in mesenchymal, epithelial and hematopoietic tumor types. Synergistic with other cytotoxic, hormonal and targeted anti-cancer therapy.</p>

<p>Acecelofenac is a non-steroidal anti-inflammatory drug that is used in the treatment of osteoarthritis, arthritis, and ankylosing spondylitis. This drug is also a cyclooxygenase inhibitor and works by inhibiting this enzyme so that pain and inflammation is reduced.</p>

<p>Inhibitor of human neutrophil elastase</p>

<p>Inhibits MET, VEGFR1-3, Tie and Ron tyrosine kinases; antineoplastic</p>

<p>Thioglycosyl Naphthalimide is a highly potent human O-GlcNAcase (hOGA) inhibitor with good selectivity against human β-N-acetylhexosaminidase B (HsHexB).</p>

<p>BRK tyrosine kinase (PTK6) inhibitor; anti-proliferative in breast cancer cells</p>

<p>Inhibitor of leucine-rich repeat kinase LRRK2Â</p>

<p>γ-secretase inhibitor; reduces amyloid-β in brainÂ</p>

<p>Specific inhibitor of the ubiquitin specific protease-7 (USP7), which is a validated deubiquitinase of the E3 ubiquitin-protein ligase MDM2. The compound inhibits the USP7 deubiquitinase activity by binding to acidic amino acid residues important for the interaction with ubiquitin. Induces tumor cell death and enhances cytotoxicity of chemotherapeutic agents.</p>

<p>Idelalisib is a pharmaceutical drug that functions as a PI3Kδ inhibitor, developed through synthetic chemical processes. Its mode of action involves selectively targeting and inhibiting phosphatidylinositol 3-kinase delta (PI3Kδ), a lipid kinase that plays a crucial role in the signaling pathways responsible for cell proliferation, survival, and differentiation. By inhibiting this enzyme, Idelalisib effectively impedes pathways that are often hyperactivated in certain hematologic malignancies, thereby exerting antitumor effects.</p>

<p>SIRT1 activator</p>

<p>Inhibitor of isocitrate dehydrogenase 2</p>

<p>Inhibits multiple tyrosine kinases (Abl1, Src family kinases, Tie-2 and VEGFR-2)</p>

<p>Inhibitor of TGF-α, CTGF, ERK1/2, NF-κB and FasL; anti-inflammatory</p>

<p>Dual inhibitor of the adaptor protein 2-associated kinase 1 (AAK1) and BMP2-inducible kinase (BMP2K) with IC50 values of 270 nM and 1 μM, respectively. In a recent study, SGC AAK1 1 stabilised β-catenin, inhibited phosphorylation of the AP2 complex subunit mu protein (AP2M1) and activated Wnt signalling in in vitro experiments._x000D_</p>

<p>Ebselen is a non-toxic organoselenium compound with antioxidant, anti-inflammatory and cytoprotective properties. Ebselen is an inhibitor of lipoxygenases, nitric oxide (NO) synthases, protein kinase C, H+/K+-ATPase, thioredoxin reductase and NADPH oxidase. Recently, ebselen has been identified by several studies as a covalent inhibitor of the main protease Mpro from coronaviruses. For the SARS-CoV-2 main protease Mpro, the IC50 value is 0.67 μM and EC50 is 4.57 μM.</p>

<p>Short acting monoamine oxidase inhibitor</p>

<p>Inhibitor of BACE1 protease</p>

<p>Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties.</p>